Abstract: A process for preparing the (R) stereoisomer of 2,2-bis(hydroxmethyl)-tetrahydrofuran monobutyrate comprising subjecting the dibutyric ester of the 2,2-bis(hydroxymethyl)-tetrahydrofuran to enzymatic hydrolysis. The invention also relates to the novel (R) stereoisomer prepared by the instant process and to its more stable forms. In addition, the invention relates to the use of the (R) stereoisomer in preparing stereoisomers of pharmacologically active compounds and to certain specific stereoisomers produced thereby.

Abstract: The invention discloses certain heterocyclic, thioether, keto-ester and alkyl phospholipids, e.g., heterocyclic phospholipids having the formula ##STR1## where R is n-C.sub.14 -C.sub.20 alkyl or O-n-C.sub.14 -C.sub.20 alkyl; each R.sub.1 is methyl or ethyl; n is 2-6; and X is --CH.sub.2 --m, where m is 2-4, CH.sub.2 CH.sub.2 O or CH.sub.2 CH.sub.2 S, or a corresponding hydrate thereof, which compounds are useful in treating multiple sclerosis.

Abstract: A process for preparing the (R) stereoisomer of 2,2-bis(hydroxmethyl)-tetrahydrofuran monobutyrate comprising subjecting the dibutyric ester of the 2,2-bis(hydroxymethyl)-tetrahydrofuran to enzymatic hydrolysis. The invention also relates to the novel (R) stereoisomer prepared by the instant process and to its more stable forms. In addition, the invention relates to the use of the (R) stereoisomer in preparing stereoisomers of pharmacologically active compounds and to certain specific stereoisomers produced thereby.

Abstract: An improved process for preparing the R- and S-isomers of 2-hydroxymethyl-2-octadecyloxymethyl-tetrahydrofuran, a critical step of which involves the preparation of the R- and S-isomers of 2-[3-(1-methoxy-1-methylethoxy)]propyl-oxiranemethanol employing metal-catalyzed Sharpless epoxidation. In addition, the invention relates to the use of the R- and S-isomers of 2-hydroxymethyl-2-octadecyloxymethyl-tetrahydrofuran in preparing stereoisomers of pharmacologically active compounds, and to the R- and S-isomers of 2-[3-(1-methoxy-1-methylethoxy)]-propyl-oxiranemethanol as novel compounds.

Abstract: The invention discloses certain thioether, keto-ester and alkyl phospholipids which are useful in treating multiple sclerosis.

Abstract: The invention discloses certain 5-aryl-substituted-2,3-dihydro-imidazo[1,2-a]furo- and thieno pyridines useful as PAF receptor antagonists and for treating tumors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-mediated bronchoconstriction and extravasation, for controlling hyperreactive airways, for protecting against endotoxin-induced hypotension and death and for treating tumors.

Abstract: The invention discloses the use of the R-(+)-isomer of 2-methoxy-3-octadecyloxy-propanol-(1)-phosphoric acid, monocholine ester in treating multiple sclerosis and to pharmaceutical compositions containing said isomer.

Abstract: invention relates to heterocyclic phospholipids of formula III which are useful in treating multiple sclerosis:where R .sub.2 is n-C.sub.14 -C.sub.20 alkyl;each R.sub.1, independently, is methyl or ethyl; Y is --O-- or --S--;n is an integer 2 to 6.

Abstract: An injectable pharmaceutical mixture comprises:(A) a water-oil emulsion vehicle comprising:(a) about 5 to 25% fatty acid triglycerides;(b) sufficient physiologically acceptable emulsifying agent, e.g. from about 0 to 1.2% egg phosphatides, purified; andthe balance water, with sufficient alkali metal hydroxide added to adjust to an alkaline pH: and(B) an active ingredient which is a PAF receptor inhibitor or anti-tumor agent, which is an ether or carbamoyl phospholipid salt.

Abstract: The invention discloses certain 5-aryl-substituted,2,3-dihydro-imidazo[1,2-a]furo- and thieno pyridines useful as PAF receptor antagonists and for treating tumors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-mediated bronchoconstriction and extravasation, for controlling hyperreactive airways, for protecting against endotoxin-induced hypotension and death and for treating tumors.

Abstract: The invention discloses certain 2- or 4-substituted-[2-(1H-imidazol-1-yl)ethyl]piperidines useful as anti-tumor agents, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions in treating tumors.

Abstract: The invention discloses certain 6-aryl-substituted-4H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,4]diazepines useful as PAF inhibitors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-induced blood platelet aggregation, PAF-mediated bronchoconstriction and extravasation, PAF-induced hypotension, PAF-induced ischemic bowel disease and PAF-mediated, endotoxin induced lung injury, for controlling hyperreactive airways and for protecting against endotoxin-induced hypotension and death.

Abstract: The invention discloses certain 5-hetero or aryl-substituted-imidazo[2,1-a]isoquinolines useful as platelet activating factor (PAF) receptor antagonists, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-mediated bronchoconstriction and extravassation and PAF-mediated, endotoxin-induced lung injury, and for controlling hyperreactive airways induced by PAF or allergin. In addition, the invention discloses the use of a select group of said compounds as anti-tumor agents.

Abstract: An improved process for preparing monoalkylcarbamate group-containing compounds comprising reacting a hydroxy group-containing compound with an organic halide and an alkali metal cyanate in the conjoint presence of a phase transfer catalyst and a solvent.

Abstract: The invention discloses certain diaryl substituted cyclopentane and cyclopentene derivatives useful as PAF inhibitors, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for inhibiting PAF-induced blood platelet aggregation, PAF-mediated broncho-constriction and extravasation, PAF-induced hypotension, PAF-induced ischemic bowel disease and PAF-mediated, endotoxin induced lug injury.

Abstract: Trifluoromethyl substituted tetracyclic compounds including optical isomers thereof having the formula: ##STR1## wherein n is 1 or 2 and p is 0 or 1, are useful as CNS agents with tranquilizing effects.

Abstract: The invention discloses substituted 2-[hydroxy(tetrahydro)-5-oxo-(2- and 3-furanyl or 2-thienyl) alkoxyphosphinyloxy]-alkanaminium hydroxide inner salt-4-oxides useful as anti-tumor agents, pharmaceutical compositions containing said compounds as an active ingredient thereof and a method of using such compositions for treating tumors.

Abstract: Amines are substituted, e.g. alkylated, by reacting the unsubstituted amine with a ketone or aldehyde, a borohydride and a rigid acid.

Abstract: Tranquilizers are of the formula I: ##STR1## wherein R.degree. is hydrogen, halo of atomic weight of from 18 to 80, i.e. fluoro, chloro or bromo, or alkyl of 1 to 3 carbon atoms,R is hydrogen, halo of atomic weight of from 18 to 80, alkyl of 1 to 4 carbon atoms, nitro or trifluoromethyl,n is 0 or 1,R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen or alkyl of 1 or 2 carbon atoms, with the proviso that no more than 2 of R.sub.1, R.sub.2 and R.sub.3 are other than hydrogen,Z is ##STR2## R' is hydrogen or alkyl of 1 or 2 carbon atoms, Y.degree. is hydrogen, halo of atomic weight of from 18 to 80 or alkyl of 1 to 3 carbon atoms,Y is hydrogen, halo of atomic weight of from 18 to 80, alkyl of 1 to 4 carbon atoms, trifluoromethyl or nitro,p is 1 or 2,q is 0, 1 or 2, andm is 0, 1, 2, 3 or 4.

Abstract: Tranquilizers are of the formula: ##STR1## wherein R.degree. is alkyl of 1 to 8 carbon atoms, andn is 1 or 2.